IngentaConnect Sitagliptin, a DPP-4 inhibitor for the treatment of patients with...

Abstract:

Background: Dipeptidyl peptidase-4 (DPP-4) inhibitors are a new class of oral antihyperglycemic agents that enhance the body's ability to regulate blood glucose by increasing the active levels of incretins, glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP). There are numerous DPP-4 inhibitors in development with sitagliptin as the first approved agent for the treatment of patients with type 2 diabetes.

Objective: The purpose of this review is to provide an overview of the clinical trial results with sitagliptin.

Methods: Clinical trials published between January 2005 (first sitagliptin publication) and November 2007 were included in this review. Medline was searched using the search terms: MK-0431 or sitagliptin.

Findings: Sitagliptin, an oral, once-daily, and highly selective DPP-4 inhibitor, has been evaluated in clinical trials as monotherapy, as add-on therapy, or as initial combination therapy with metformin. Sitagliptin provided effective fasting and postprandial glycemic control in a wide range of patients with type 2 diabetes. Markers of β-cell function (HOMA-β and proinsulin/insulin ratio) were improved with sitagliptin treatment. In these clinical trials, sitagliptin was generally well tolerated with an overall incidence of adverse experiences comparable to placebo, a low risk of hypoglycemia or gastrointestinal adverse experiences, and a neutral effect on body weight. The findings presented in this review are limited to the specific patient population enrolled in each clinical trial and for durations for up to 1 year. Future clinical studies should evaluate whether this class of agents has the potential to delay progression and/or prevent type 2 diabetes.

Conclusions: Sitagliptin has been shown to be effective and well-tolerated in various treatment regimens and may be considered for both initial therapy and as add-on therapy for patients with type 2 diabetes.

Keywords: DPP-IV; GLYCEMIC CONTROL; INCRETINS; MK-0431; TYPE 2 DIABETES

Document Type: Review article

DOI: 10.1185/030079908X261069

Affiliations: 1: Chaim Sheba Medical Center, Tel Hashomer, Israel 2: Colombian Diabetes Association, Bogotá, Colombia 3: Merck Research Laboratories, Rahway, NJ, USA

The full text article is available for purchase

$31.50 plus tax

Sitagliptin, a DPP-4 inhibitor for the treatment of patients with type 2 diabetes: a review of recent clinical trials